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Results for "

inward+current

" in MedChemExpress (MCE) Product Catalog:

24

Inhibitors & Agonists

3

Peptides

3

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-A0170
    Trovafloxacin
    5+ Cited Publications

    		 Bacterial Topoisomerase Antibiotic Infection
    Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
    Trovafloxacin
  • HY-103399
    Trovafloxacin mesylate
    5+ Cited Publications

    		 Bacterial Topoisomerase Antibiotic Infection
    Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
    Trovafloxacin mesylate
  • HY-12882A
    Ifenprodil tartrate
    5+ Cited Publications

    NP-120 tartrate; RC-61-91 tartrate

    		 iGluR Adrenergic Receptor Potassium Channel Calcium Channel Influenza Virus Infection Neurological Disease
    Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
    Ifenprodil tartrate
  • HY-118504
    Sulfoxaflor
    1 Publications Verification

    		 Environmental Pollutants nAChR Neurological Disease
    Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .
    Sulfoxaflor
  • HY-13422
    Zatebradine hydrochloride
    2 Publications Verification

    UL-FS-49; UL-FS-49CL

    		 HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
    Zatebradine hydrochloride
  • HY-12882
    Ifenprodil
    Maximum Cited Publications
    10 Publications Verification

    NP-120; RC-61-91

    		 iGluR Adrenergic Receptor Potassium Channel Calcium Channel Influenza Virus Infection Neurological Disease
    Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease .
    Ifenprodil
  • HY-135783
    AT 1001
    1 Publications Verification

    		 nAChR Neurological Disease Metabolic Disease Inflammation/Immunology
    AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
    AT 1001
  • HY-N6868
    Dimethyl lithospermate B

    dmLSB

    		 Sodium Channel Cardiovascular Disease
    Dimethyl lithospermate B (dmLSB) is a selective Na + channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP) .
    Dimethyl lithospermate B
  • HY-13422A
    Zatebradine
    2 Publications Verification

    UL-FS-49 free base; UL-FS-49CL free base

    		 HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
    Zatebradine
  • HY-19434
    trans-ACPD

    Trans-(±)-ACP

    		 mGluR Metabolic Disease
    trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
    trans-ACPD
  • HY-108960
    PPADS

    		P2X Receptor Interleukin Related Neurological Disease
    PPADS is a P2X receptor (P2X Receptor) antagonist and a reversible competitive antagonist of NAADP receptors, with IC50 values of 68 nM (P2X1) and 214 nM (P2X3), respectively. PPADS alleviates pain-related behaviors in the central and peripheral nervous systems of mice after peripheral neuropathy, inhibits the overproduction of IL-1β, IL-6, iNOS and nNOS, and suppresses the hydrolytic activity of extracellular ATPase. PPADS blocks ATP-mediated inward currents on recombinant rat P2X1 and P2X3 receptors, and inhibits purinergic nerve stimulation-induced contraction of rabbit bladder detrusor muscle. PPADS is applicable to research related to neuropathic pain .
    PPADS
  • HY-137325A
    2-Chloro-ATP sodium

    		Calcium Channel Metabolic Disease
    2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
    2-Chloro-ATP sodium
  • HY-103298
    MNI-caged kainate

    		Endogenous Metabolite Neurological Disease
    MNI-caged kainate is a photoprotected neuroactive amino acid with the activity to generate large inward currents. MNI-caged kainate can be released at the resting membrane potential of Purkinje cells and generate significant inward currents. The release of MNI-caged kainate results in approximately 40% of the current being generated through AMPA receptor activation. MNI-caged kainate is used to study fast synaptic receptor mechanisms. The photorelease time of MNI-caged kainate is in the sub-microsecond range, making it suitable for investigating the mechanisms of fast synaptic transmission .
    MNI-caged kainate
  • HY-116072
    Antiarrhythmic agent-2

    		Calcium Channel Cardiovascular Disease
    Antiarrhythmic agent-2 is a nonspecific Ca 2+ inward current blocker that inhibits ionic currents in sensory neuron membranes. Antiarrhythmic agent-2 can be used in the study of cardiovascular diseases, such as arrhythmias .
    Antiarrhythmic agent-2
  • HY-107717
    MNI-caged-NMDA

    		iGluR Neurological Disease
    MNI-caged-NMDA is a light-sensitive amino acid with rapid release properties suitable for use in the study of fast synaptic receptor mechanisms. MNI-caged-NMDA shows metered release of NMDA receptors, inducing rapid and sustained receptor activation in cerebellar interneurons. MNI-caged-NMDA is able to achieve rapid transient responses and generate large inward currents by local laser photolysis. The use of MNI-caged-NMDA can effectively study neurotransmitter signaling and its inhibitory effects on GABA-A receptors .
    MNI-caged-NMDA
  • HY-13422R
    Zatebradine hydrochloride (Standard)

    UL-FS-49 (Standard); UL-FS-49CL (Standard)

    		 HCN Channel Reference Standards Cardiovascular Disease
    Zatebradine (hydrochloride) (Standard) is the analytical standard of Zatebradine (hydrochloride). This product is intended for research and analytical applications. Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 μM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 μM, 2.21 μM, 1.90 μM and 1.88 μM, respectively .
    Zatebradine hydrochloride (Standard)
  • HY-118814
    YM928

    		iGluR Neurological Disease
    YM928 is an orally active and noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. YM928 inhibits AMPA receptor-mediated toxicity in primary rat hippocampal cultures with an IC50 value of 2 μM. YM928 blocks AMPA-induced intracellular calcium influx with an IC50 value of 3 μM and antagonizes AMPA-induced inward currents with an IC50 value of 1 μM. YM928 is promising for research of neurological disorders .
    YM928
  • HY-118504S
    Sulfoxaflor-d3

    		Isotope-Labeled Compounds nAChR Neurological Disease
    Sulfoxaflor-d3 is the deuterium labeled Sulfoxaflor (HY-118504). Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .
    Sulfoxaflor-d3
  • HY-A0170R
    Trovafloxacin (Standard)

    		Reference Standards Bacterial Topoisomerase Antibiotic Infection
    Trovafloxacin (Standard) is the analytical standard of Trovafloxacin. This product is intended for research and analytical applications. Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
    Trovafloxacin (Standard)
  • HY-18940
    Cilobradine

    Cilo

    		 Endogenous Metabolite Cardiovascular Disease
    Cilobradine (Cilo) is a HCN channel blocker with heart rate reducing activity. Cilobradine blocks the slow inward current of human HCN1, HCN2, HCN3, and HCN4 channels. Cilobradine has a slightly higher efficiency in blocking endogenous If in mouse sinoatrial node cells (IC50 value is 0.62μM). Cilobradine can dose-dependently reduce the heart rate from 600 to 200 bpm with an ED50 value of 1.2 mg/kg. Cilobradine induces arrhythmias at doses greater than 5 mg/kg, which are characterized by periodic fluctuations between T waves and P waves .
    Cilobradine
  • HY-12882AR
    Ifenprodil tartrate (Standard)

    NP-120 tartrate (Standard); RC-61-91 tartrate (Standard)

    		 iGluR Potassium Channel Reference Standards Neurological Disease
    Ifenprodil (tartrate) (Standard) is the analytical standard of Ifenprodil (tartrate). This product is intended for research and analytical applications. Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
    Ifenprodil tartrate (Standard)
  • HY-132227
    Dichlorobenzamil hydrochloride

    3',4'-Dichlorobenzamil hydrochloride; L-594881 hydrochloride

    		 Na+/Ca2+ Exchanger Others
    Dichlorobenzamil (3',4'-Dichlorobenzamil; L-594881) hydrochloride is a Na +-Ca 2+ Exchanger inhibitor. Dichlorobenzamil (hydrochloride) attenuates the Na +-Ca 2+ exchanger-mediated inward current induced by activation of type I metabotropic glutamate receptors in second-order baroreceptor neurons of the rat nucleus tractus solitarius .
    Dichlorobenzamil hydrochloride
  • HY-P1278B
    GR 64349 acetate

    		Neurokinin Receptor Neurological Disease Endocrinology
    GR 64349 acetate is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 acetate selectively activates the NK-2 receptor subtype. GR 64349 acetate activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 acetate does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 acetate induces inward currents .
    GR 64349 acetate
  • HY-185007
    LI-633

    		GABA Receptor Neurological Disease
    LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a Ki of 21 nM. LI-633 produces robust potentiation of GABA-induced inward current, with EC50 values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 potentiates muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons with an EC50 of 70.4 nM. LI-633 can be used for the study of visceral pain .
    LI-633

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